Synthesis and Biological Evaluation of Novel 99mTc-Labelled Bisphosphonates as Superior Bone Imaging Agents

Molecules

Ling Qiu¹  Wen Cheng¹  Jianguo Lin¹  Shineng Luo¹  Li Xue¹ 

[1] Key Laboratory of Nuclear Medicine, Ministry of Health, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China

关键词: zoledronic acid derivative;    ^99mTc-labelled diphosphonates;    in vitro stability;    biodistribution;    bone imaging agent;   

DOI  :  10.3390/molecules16086165

来源: mdpi

【 摘 要 】

A series of novel zoledronic acid (ZL) derivatives 1-hydroxy-3-(2-methyl-1H-imidazol-1-yl)propane-1,1-diyldiphosphonic acid (MIPrDP), 1-hydroxy-4-(2-methyl-1H-imidazol-1-yl)butane-1,1-diyldiphosphonic acid (MIBDP), and 1-hydroxy-5-(2-methyl-1H-imidazol-1-yl)pentane-1,1-diyldiphosphonic acid (MIPeDP) were prepared and successfully labeled with ^99mTc in high labeling yields. The in vitro stability and in vivo biodistribution of ^99mTc-MIPrDP, ^99mTc-MIBDP and ^99mTc-MIPeDP were investigated and compared. The biodistribution studies indicate that the radiotracer ^99mTc-MIPrDP has highly selective uptake in the skeletal system and rapid clearance from soft tissues. The present findings indicate that ^99mTc-MIPrDP holds great potential for use in bone imaging.

【 授权许可】

CC BY   
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